49 results about "Dasatinib" patented technology

The invention discloses an application of dasatinib in preparation of a medicine for treating endometriosis. The dasatinib can be used for treating endometriosis. The new application of the dasatinib in treating the endometriosis has important clinical significance on accurate treatment of the endometriosis.

The invention discloses a micro-flow field preparation method of dasatinib nanocrystals. The method comprises the following steps: dissolving dasatinib in an organic solvent to serve as a solvent phase A; dissolving a surfactant in deionized water to serve as an anti-solvent phase B, simultaneously pumping the solvent phase A and the anti-solvent phase B into a micro-flow field device for full reaction, collecting dasatinib crystal dispersion liquid at an outlet, centrifuging to remove supernate, taking bottom precipitate, and performing vacuum drying to obtain the solid nanocrystal. According to the present invention, the micro-flow field device is adopted, the mixing process of the solvent and the anti-solvent is enhanced, the surfactant is adopted as the dispersant, the transport efficiency and the supersaturation degree of the drug molecules are regulated and controlled, the efficient preparation of the dasatinib nanocrystal is achieved, the operation is simple, the reaction speed is fast, and the safety is high.

Amorphous solid dispersions and pharmaceutical compositions of the protein kinase inhibitor dasatinib. The pharmaceutical compositions may be used in methods of treating a proliferative disorder such as cancer, or in methods of delivering dasatinib to patients without regard to whether the patient is concurrently administered a gastric acid-reducing agent, or without regard to whether the patient has an elevated gastric pH. The compositions may be particularly suitable for patients afflicted by achlorhydria or hypochlorhydria, or Helicobacter pylori infection.

The present invention relates to the prevention or mitigation of adverse reactions associated with gene therapy, such as the formation of anti-drug antibodies. In particular, the present invention relates to the use of tyrosine kinase inhibitors, such as dasatinib, to prevent or ameliorate such side effects.

According to the invention, a polymer prodrug is designed and prepared, and a dasatinib (DAS) and triphenylphosphine-adriamycin (TPP-DOX, TD) co-loaded nano-micelle is constructed; the preparation method has the advantages that 1) the optimal preparation process of the polymer micelle is determined by a single factor investigation method, namely the optimal nano-micelle is prepared by using a dialysis method and taking DMF (Dimethyl Formamide) as a solvent according to the mass ratio of a prodrug material to a carried drug being 15: 1, and the preparation method is simple and clear and is easy to industrialize; 2) the particle size is small and uniform, so that the nanoparticles can be enriched at a tumor part through an EPR effect; 3) the amphiphilic micromolecule prodrug improves the water solubility of DAS, improves the drug stability, has high drug loading capacity, and avoids adverse reactions possibly caused by carriers and auxiliary materials; and 4) the polymer nano-micelle co-loaded with the DAS and the TPP-DOX has good MMP-2 sensitive responsiveness, enhances the drug targeting delivery capability, has good blood compatibility and safety, improves the drug curative effect, reduces the toxic and side effects, and has a good tumor MDR reversing effect.

Amorphous solid dispersions and pharmaceutical compositions of the protein kinase inhibitor dasatinib. The pharmaceutical compositions may be used in methods of treating a proliferative disorder such as cancer, or in methods of delivering dasatinib to patients without regard to whether the patient is concurrently administered a gastric acid-reducing agent, or without regard to whether the patient has an elevated gastric pH. The compositions may be particularly suitable for patients afflicted by achlorhydria or hypochlorhydria, or Helicobacter pylori infection.

The invention belongs to the field of biological medicine, and particularly relates to a nano-drug based on chondroitin sulfate as well as a preparation method and application of the nano-drug. Chondroitin sulfate (CS) and dasatinib (DAS) are connected through a GFLG connexon responded by cathepsin B (CTSB) to prepare the prodrug CS-GFLG-DAS (CGD), the prodrug CS-GFLG-DAS (CGD) is used for reversing the phenotype of cancer-related fibroblasts and reducing the biosynthesis of extracellular matrixes, fibrotic tumors are efficiently treated, and a new perspective is provided for optimizing the application of immunotherapy in fibrotic tumors.

The invention belongs to the field of pharmaceutical preparations, and particularly relates to a dalcotinib pharmaceutical composition and a preparation method thereof.The dalcotinib pharmaceutical composition is prepared from, by weight, 10-30 parts of dalcotinib, 25-60 parts of lactose, 25-60 parts of microcrystalline cellulose, 1-15 parts of carboxymethyl starch sodium and 0.5-5 parts of magnesium stearate; the average particle size D50 of the lactose is greater than or equal to 120 microns. The dalcotinib composition disclosed by the invention is high in dissolution rate, quick in disintegration, good in fluidity, capable of avoiding sticking, good in dissolution rate stability and simple in preparation process.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to a dasatinib vanillic acid crystal form and a preparation method thereof, and in the dasatinib vanillic acid crystal form provided by the invention, the molar ratio of dasatinib to vanillic acid to water is 1: 1: 1. The dasatinib vanillic acid crystal form provided by the invention has relatively good stability and relatively high dissolution rate, and is of great significance for improving the bioavailability of a dasatinib medicine and preparing a preparation.

The invention belongs to the technical field of biological medicines, and discloses application of dasatinib in preparation of a medicine for promoting retina ganglion cell axon regeneration and dendritic repair. The research of the invention finds that dasatinib has the effect of promoting RGC axon regeneration and dendritic repair after optic nerve injury. When dasatinib is adopted for treatment, repair and regeneration of retinal ganglion cell axons and dendrites after optic nerve injury can be promoted, and the purpose of treating traumatic optic nerve injury is achieved.

The invention provides an NO donor type dasatinib derivative as well as a preparation method and application thereof. The derivative is one of a compound 1a-1f and a compound 2a-2f; the derivative has multiple effects of removing senescence cells, reducing intraocular pressure and protecting optic nerves, and is a novel potential treatment medicine for treating glaucoma and senescence-related retinopathy.

The invention relates to an application of a dasatinib and quercetin pharmaceutical composition in preparation of a medicine for improving the outcome of elderly adverse pregnancy, belongs to the technical field of biological medicines, and particularly discloses an application of the dasatinib and quercetin pharmaceutical composition. The technical problem of placenta dysfunction caused by elderly pregnancy is solved. The dasatinib and the quercetin form the pharmaceutical composition, so that the autophagy activity of trophoblasts is promoted, DNA (deoxyribonucleic acid) damaged cells are eliminated, the adverse pregnancy outcome caused by the elderly is remarkably improved, the embryo absorption rate is reduced by about 10%, and the weight of a fetus is increased by about 20mg. The invention provides a new targeted intervention strategy for the outcome of elderly adverse pregnancy.

Amorphous solid dispersions and pharmaceutical compositions of the protein kinase inhibitor dasatinib. The pharmaceutical compositions may be used in methods of treating a proliferative disorder such as cancer, or in methods of delivering dasatinib to patients without regard to whether the patient is concurrently administered a gastric acid-reducing agent, or without regard to whether the patient has an elevated gastric pH. The compositions may be particularly suitable for patients afflicted by achlorhydria or hypochlorhydria, or Helicobacter pylori infection. The compositions may be administered intact, or may be crushed prior to administration.

Combination therapies for use in the treatment of brain tumours, particularly glioma and embryonal brain tumours. Disclosed herein are pharmaceutical compositions comprising a complex of Panobinostat and a cyclodextrin, a second pharmaceutical agent, and a pharmaceutically acceptable excipient, diluent or carrier, in which the second pharmaceutical agent is Niclosamide, Dasatinib or Duvelisib. Associated methods of treatment and use are further disclosed.

Described herein are methods useful for the treatment of cancers in a canine subject with a pharmaceutical compositions comprising HDAC inhibitors, Rapamycin, Dasatinib, Lapatinib, Trametinib, Vorinostat, Imatinib, Crizotinib, Sorafenib, and combinations thereof. Also described herein are methods for identification of subjects with cancers that will benefit from administration of the pharmaceutical compositions comprising HIDAC inhibitors, Rapamycin, Dasatinib, Lapatinib, Trametinib, Vorinostat, Imatinib, Crizotinib, Sorafenib, and combinations thereof. In certain aspects, the methods described herein further comprise administering a therapeutically effective amount of at least one additional anti-cancer agent.

Provided herein are methods for inactivating effector cells (e.g., NK cells, including cells as spot type cells for adoptive cell therapy). The inactivated cells can be cryopreserved after inactivation. The inactivated cells may be expanded and / or activated prior to inactivation, and may or may not include a transgene, which may optionally encode a chimeric antigen receptor and / or a T cell receptor. In certain embodiments, disclosed are methods for inactivating NK cells comprising treating with an inactivating agent, which is a kinase inhibitor, such as an mTOR inhibitor, and / or a tyrosine kinase inhibitor, such as rapamycin and / or dasatinib. Also provided herein are inactivated and cryopreserved NK cells, and methods of making and / or using the same for treating a subject in need thereof (e.g., treating a subject having cancer).

The application discloses a kind of synthesis method of dasatinib intermediate in the field of organic synthesis, with 2-aminothiazole-4-carboxylic acid as raw material, first and tert-pivaloyl chloride in situ generates mixed anhydride, further and 2-chloro-6-methylaniline condensation reaction occurs after, the compound 2 obtained is not separated directly hydrolyzed to obtain high-purity 2-amino-N-(2-chloro-6-methylphenyl) thiazole-5-formamide.Due to the mixed anhydride formed by tert-pivaloyl chloride has greater steric hindrance, and the further reaction of corresponding amine is conducive to the regioselectivity, and by-product tert-pivalic acid can be easily removed by post-treatment, so as to solve the disadvantages existing in the prior art, the unit operation involved in the whole preparation process is simpler, and the product purity and yield are higher, with good application prospect.

Methods for the treatment of cancer, including glioblastoma multiforme (GBM) and recurrent glioblastoma multiforme (RGBM). The method includes administering to a patient a plurality of extraneous antineoplastons and a plurality of targeted agents. The plurality of extraneous antineoplastons may include two or more antineoplastons selected from phenylacetylglutaminate sodium (PG), phenylacetylisoglutaminate sodium (iso-PG), and phenylacetate (PN). The plurality of targeted agents may include two or more agents selected from bevacizumab, pazopanib, sorafenib, dasatinib, and everolimus.

The present invention relates to combination therapies for treating KRas G12C cancers. In particular, the present invention relates to methods of treating cancer in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a combination of a Src-family kinase inhibitor and a KRAS G12C inhibitor of Formula (I), Formula I-A or Formula I-B, pharmaceutical compositions comprising a therapeutically effective amounts of the inhibitors, kits comprising the compositions and methods of use therefor.

Provided herein are methods for deactivation of effector cells, such as NK cells, including cells for adoptive cell therapy that are off-the-shelf cells. The deactivated cells may be cryopreserved following deactivation. The deactivated and cell may be expanded and / or activated prior to deactivation, and may or may not comprise a transgene, which may optionally encode a chimeric antigen receptor and / or T cell receptor. In certain embodiments, disclosed are methods for deactivation of NK cells comprising treatment with a kinase inhibitor, for example an mTOR inhibitor and / or a tyrosine kinase inhibitor, for example rapamycin and / or Dasatinib. Also provided herein are deactivated and cryopreserved NK cells, and methods of preparing and / or using the same for treatment of a subject in need thereof, for example treatment of a subject with cancer.

Amorphous solid dispersions and pharmaceutical compositions of the protein kinase inhibitor dasatinib. The pharmaceutical compositions may be used in methods of treating a proliferative disorder such as cancer, or in methods of delivering dasatinib to patients without regard to whether the patient is concurrently administered a gastric acid-reducing agent, or without regard to whether the patient has an elevated gastric pH. The compositions may be particularly suitable for patients afflicted by achlorhydria or hypochlorhydria, or Helicobacter pylori infection.

The present application relates to the m 6 Application of methylation level of A as glioma marker, the present application confirms the m 6 The methylation modification level is related to the prognosis condition of brain glioma, and the increase of methylation abundance and expression level means worse prognosis. In addition, the present application researches and confirms that the expression of lncRNA-WEE2-AS1 is related to the formation of drug resistance of anti-tumor drugs, and inhibiting the expression of the lncRNA helps to improve the resistance of dasatinib, and provides a feasible treatment scheme for the clinical targeted treatment of drug-resistant patients.

[Method for reprogramming type 1 alveolar cells into type 2 alveolar cells using Rhosin] The present invention relates to a composition for inducing the reprogramming of type 1 alveolar cells into type 2 alveolar cells, the composition containing Rhosin as an active ingredient. According to the present invention, it is expected to be possible not only to reprogram AT1 cells into AT2 cells using Rhosin and thereby efficiently obtain AT2 cells which were previously difficult to obtain in sufficient numbers, but also to reprogram AT1 cells into AT2 cells in organoids while culturing the organoids themselves rather than culturing single cells, and thereby obtain cells having physiological activity more similar to that of actual tissue. [Method for reprogramming type 1 alveolar cells into type 2 alveolar cells using Dasatinib] The present invention relates to a composition for inducing the reprogramming of type 1 alveolar cells into type 2 alveolar cells, the composition containing Dasatinib as an active ingredient. According to the present invention, it is expected to be possible not only to reprogram AT1 cells into AT2 cells using Dasatinib and thereby efficiently obtain AT2 cells which were previously difficult to obtain in sufficient numbers, but also to reprogram AT1 cells into AT2 cells in organoids while culturing the organoids themselves rather than culturing single cells, and thereby obtain cells having physiological activity more similar to that of actual tissue. [Method for reprogramming type 1 alveolar cells into type 2 alveolar cells using ML141] The present invention relates to a composition for inducing the reprogramming of type 1 alveolar cells into type 2 alveolar cells, the composition containing ML141 as an active ingredient. According to the present invention, it is expected to be possible not only to reprogram AT1 cells into AT2 cells using ML141 and thereby efficiently obtain AT2 cells which were previously difficult to obtain in sufficient numbers, but also to reprogram AT1 cells into AT2 cells in organoids while culturing the organoids themselves rather than culturing single cells, and thereby obtain cells having physiological activity more similar to that of actual tissue. [ML141-containing composition for inhibiting lung cancer metastasis] The present invention relates to a composition for inhibiting lung cancer metastasis, the composition containing ML141 as an active ingredient. [Dasatinib-containing composition for inhibiting lung cancer metastasis] The present invention relates to a composition for inhibiting lung cancer metastasis, the composition containing Dasatinib as an active ingredient.

The present invention discloses a method for regulating CAR-T cells and its application. The present invention regulates CAR-T cells through tyrosine kinase inhibitors, thereby alleviating and treating immune-related toxicities that may occur after CAR-T cells are used for treatment. The regulation method of the present invention can regulate the expression of various cytokines related to CAR-T cell immunotoxicity, perform early intervention on related toxicities, reduce the incidence and mortality of severe toxicities, and thus improve the safety of CAR-T cells. Dasatinib in the regulation method used in the present invention is an anti-tumor drug that has been approved for clinical treatment and can be applied in the treatment of various cancers, enabling the reuse of old drugs and having great economic value.

To provide an amorphous solid dispersion ("ASD") comprising dasatinib, a pharmaceutical composition comprising ASD, and a method of treatment comprising administration of the pharmaceutical composition.SOLUTION: Amorphous solid dispersions and pharmaceutical compositions of the protein kinase inhibitor dasatinib. The pharmaceutical compositions can be used in methods of treating a proliferative disorder, such as cancer, or in methods of delivering dasatinib to a patient regardless of whether the patient is concurrently using a gastric acid reducing agent or the patient has an elevated gastric pH. The composition may be particularly suitable for patients suffering from achlorhydria or hypoacidity, or Helicobacter pylori infection.SELECTED DRAWING: Figure 7

This invention belongs to the field of biotechnology and relates to the application of an inhibitor blocking the TRIB3 / SRC interaction, alone or in combination with an SRC kinase inhibitor, in the preparation of drugs for the prevention or treatment of pancreatic cancer, breast cancer, liver cancer, and kidney cancer. Specifically, it discloses an inhibitor that overcomes resistance to traditional small molecule drugs and targets tumor migration and stemness by blocking the TRIB3 / SRC interaction, and its application, alone or in combination with an SRC kinase inhibitor, in the preparation of drugs for the prevention or treatment of pancreatic cancer, breast cancer, liver cancer, and kidney cancer. The amino acid sequence of the TRIB3 / SRC kinase inhibitor is listed in SEQ ID No. 1, and the SRC kinase inhibitor is Dasatinib. We found that this peptide can promote the degradation of TRIB3 and SRC, inhibit tumor migration and stemness, and inhibit tumor development and progression. Combined use with an SRC kinase inhibitor shows significant efficacy, and therefore it is applied in the preparation of drugs for the treatment and prevention of pancreatic cancer, breast cancer, liver cancer, and kidney cancer. The prepared drugs show significant efficacy in treating tumor diseases, with few toxic side effects and high safety, and have promising development prospects.

The invention discloses application of dasatinib and quercetin in prevention and treatment of osteomyelitis. The dasatinib and the quercetin can effectively eliminate cell senescence of Adipoq + myofibroblasts around medullary cavity abscess. Therefore, blood perfusion and antibiotic permeation around the abscess are increased, local blood perfusion around the abscess is improved, the bacterial load is reduced, the bone mass and bone microstructure of the staphylococcus aureus osteomyelitis are improved, and the method is a potential effective treatment strategy for preventing and treating the pathological progress of the staphylococcus aureus osteomyelitis.

The present invention discloses a cell membrane nanoparticle and its preparation method and use. + T cells, cell membrane nanoparticles TaCD4M1-NP with ROS response. This nanoparticle can carry CD4 + T cells infiltrate the inflammatory site and rely on the membrane proteins of the cell membrane to achieve enrichment and retention in the inflammatory site, increase the drug concentration in the target site, and reduce toxic and side effects. By selecting a combination of anti-inflammatory drugs, methotrexate and dasatinib were selected for combined administration. The results showed that the combination had synergistic efficacy in various inflammatory models. Cell membrane nanoparticles loaded with MTX and DAS can effectively carry CD4 + T cells, which infiltrate inflammatory sites such as the colon in ulcerative colitis (UC) and the joints in rheumatoid arthritis (RA), significantly enhance the efficacy of drugs against UC and RA, providing a new approach for the treatment of inflammatory diseases.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to a dasatinib fumaric acid crystal form and a preparation method thereof, and in the dasatinib fumaric acid crystal form provided by the invention, the molar ratio of dasatinib to fumaric acid to methanol is 1: 1: 1. The dasatinib fumaric acid crystal form provided by the invention has relatively good stability and relatively high dissolution rate, and is of great significance for improving the bioavailability of a dasatinib medicine and preparing a preparation.